WDR5-0102 is a selective inhibitor of the WDR5-MLL1 complex, exhibiting a dissociation constant (Kd) of 4 μM and a competitive inhibition constant (Kdis) of 7 μM. This compound effectively suppresses the H3K4 methyltransferase activity of MLL1 without affecting other human methyltransferases, including SETD7 and several others such as G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5. WDR5-0102 is a valuable tool for investigating the role of MLL1 in various biological processes and its implications in cancer research.
WDR5-0102 is a selective inhibitor of the WDR5-MLL1 complex, exhibiting a dissociation constant (Kd) of 4 μM and a competitive inhibition constant (Kdis) of 7 μM. This compound effectively suppresses the H3K4 methyltransferase activity of MLL1 without affecting other human methyltransferases, including SETD7 and several others such as G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5. WDR5-0102 is a valuable tool for investigating the role of MLL1 in various biological processes and its implications in cancer research.
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